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Siegel, R. A.; Kapoor, M.; Cheryala, N.; Georg, G. I.; Cloyd, J. C. Water-soluble benzodiazepine prodrug/enzyme combinations for intranasal rescue therapies. Epilepsy Behav 2015, 49, 347-350.

Olesen, S. H.; Ingles, D. J.; Zhu, J. Y.; Martin, M. P.; Betzi, S.; Georg, G. I.; Tash, J. S.; Schonbrunn, E. Stability of the Human Hsp90-p50(Cdc37) Chaperone Complex against Nucleotides and Hsp90 Inhibitors, and the Influence of Phosphorylation by Casein Kinase 2. Molecules 2015, 20, 1643-1660.

Li, W.; Schneider, C. M.; Georg, G. I. Synthesis of Strained 1,3-Diene Macrocycles via Copper-Mediated Castro-Stephens Coupling/Alkyne Reduction Tandem Reactions. Org Lett 2015, 17, 3902-3905.

Li, W.; Georg, G. I. A concise formal total synthesis of lactimidomycin. Chem Commun 2015, 51, 8634-8636.

Kirtane, A. R.; Wong, H. L.; Guru, B. R.; Lis, L. G.; Georg, G. I.; Gurvich, V. J.; Panyam, J. Reformulating Tylocrebrine in Epidermal Growth Factor Receptor Targeted Polymeric Nanoparticles Improves Its Therapeutic Index. Mol Pharmaceut 2015, 12, 2912-2923.

Dahlin, J. L.; Nissink, J. W. M.; Strasser, J. M.; Francis, S.; Higgins, L.; Zhou, H.; Zhang, Z. G.; Walters, M. A. PAINS in the Assay: Chemical Mechanisms of Assay Interference and Promiscuous Enzymatic Inhibition Observed during a Sulfhydryl-Scavenging HTS. J Med Chem 2015, 58, 2091-2113.

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Dahlin, J. L.; Chen, X. Y.; Walters, M. A.; Zhang, Z. G. Histone-modifying enzymes, histone modifications and histone chaperones in nucleosome assembly: Lessons learned from Rtt109 histone acetyltransferases. Crit Rev Biochem Mol 2015, 50, 31-53.

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Yu, Y. Y.; Ranade, A. R.; Georg, G. I. Transition Metal-Free Direct Trifluoromethylation of 2,3-Dihydropyridin-4(1H)-ones at Room Temperature. Adv Synth Catal 2014, 356, 3510-3518.

Yu, Y. Y.; Georg, G. I. Biomimetic Aerobic C-H Olefination of Cyclic Enaminones at Room Temperature: Development toward the Synthesis of 1,3,5-Trisubstituted Benzenes. Adv Synth Catal 2014, 356, 1359-1369.

Seki, H.; Georg, G. I. 2,3-Dihydropyridin-4(1H)-ones and 3-Aminocyclohex-2-enones: Synthesis, Functionalization, and Applications to Alkaloid Synthesis. Synlett 2014, 25, 2536-2557.

Seki, H.; Georg, G. I. Enantiospecific Synthesis and Biological Investigations of a Nuphar Alkaloid: Proposed Structure of a Castoreum Component. Eur J Org Chem 2014, 2014, 3777-3783.

Ranade, A. R.; Georg, G. I. Enantioselective Synthesis of 3,4-Dihydro-1,2-oxazepin-5(2H)-ones and 2,3-Dihydropyridin-4(1H)-ones from beta-Substituted beta-Hydroxyaminoaldehydes. J Org Chem 2014, 79, 984-992.

Maize, K. M.; Kurbanov, E. K.; De La Mora-Rey, T.; Geders, T. W.; Hwang, D. J.; Walters, M. A.; Johnson, R. L.; Amin, E. A.; Finzel, B. C. Anthrax toxin lethal factor domain 3 is highly mobile and responsive to ligand binding. Acta Crystallogr D 2014, 70, 2813-2822.

Kim, Y. W.; Georg, G. I. Boron-Heck Reaction of Cyclic Enaminones: Regioselective Direct Arylation via Oxidative Palladium(II) Catalysis. Org Lett 2014, 16, 1574-1577.

Khatri, A.; Williams, B. W.; Fisher, J.; Brundage, R. C.; Gurvich, V. J.; Lis, L. G.; Skubitz, K. M.; Dudek, A. Z.; Greeno, E. W.; Kratzke, R. A.; Lamba, J. K.; Kirstein, M. N. SLC28A3 genotype and gemcitabine rate of infusion affect dFdCTP metabolite disposition in patients with solid tumours. British Journal of Cancer 2014, 110, 304-312.

Kapoor, M.; Winter, T.; Lis, L.; Georg, G. I.; Siegel, R. A. Rapid Delivery of Diazepam from Supersaturated Solutions Prepared Using Prodrug/Enzyme Mixtures: Toward Intranasal Treatment of Seizure Emergencies. Aaps J 2014, 16, 577-585.

Hassig, C. A.; Zeng, F. Y.; Kung, P.; Kiankarimi, M.; Kim, S.; Diaz, P. W.; Zhai, D. Y.; Welsh, K.; Morshedian, S.; Su, Y.; O'Keefe, B.; Newman, D. J.; Rusman, Y.; Kaur, H.; Salomon, C. E.; Brown, S. G.; Baire, B.; Michel, A. R.; Hoye, T. R.; Francis, S.; Georg, G. I.; Walters, M. A.; Divlianska, D. B.; Roth, G. P.; Wright, A. E.; Reed, J. C. Ultra-High-Throughput Screening of Natural Product Extracts to Identify Proapoptotic Inhibitors of Bcl-2 Family Proteins. J Biomol Screen 2014, 19, 1201-1211.

Haslach, E. M.; Huang, H. S.; Dirain, M.; Debevec, G.; Geer, P.; Santos, R. G.; Giulianotti, M. A.; Pinilla, C.; Appel, J. R.; Doering, S. R.; Walters, M. A.; Houghten, R. A.; Haskell-Luevano, C. Identification of Tetrapeptides from a Mixture Based Positional Scanning Library That Can Restore nM Full Agonist Function of the L106P, I69T, I102S, A219V, C271Y, and C271R Human Melanocortin-4 Polymorphic Receptors (hMC4Rs). J Med Chem 2014, 57, 4615-4628.

Ember, S. W. J.; Zhu, J. Y.; Olesen, S. H.; Martin, M. P.; Becker, A.; Berndt, N.; Georg, G. I.; Schonbrunn, E. Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors. Acs Chem Biol 2014, 9, 1160-1171.

Dosa, P. I.; Georg, G. I.; Gurvich, V. J.; Hawkinson, J. E.; Walters, M. A.; Wong, H. L. From HTS to Phase I: The Institute for Therapeutics Discovery and Development at the University of Minnesota. Combinatorial Chemistry & High Throughput Screening 2014, 17, 231-240.

Dahlin, J. L.; Walters, M. A. The essential roles of chemistry in high-throughput screening triage. Future medicinal chemistry 2014, 6, 1265-90.

Dahlin, J. L.; Kottom, T.; Han, J. H.; Zhou, H.; Walters, M. A.; Zhang, Z. G.; Limper, A. H. Pneumocystis jirovecii Rtt109, a Novel Drug Target for Pneumocystis Pneumonia in Immunosuppressed Humans. Antimicrob Agents Ch 2014, 58, 3650-3659.

Cushman, M.; Georg, G. I.; Holzgrabe, U.; Wang, S. M. Absolute Quantitative H-1 NMR Spectroscopy for Compound Purity Determination. J Med Chem 2014, 57, 9219-9219.

Chou, T. F.; Bulfer, S. L.; Weihi, C. C.; Li, K. L.; Lis, L. G.; Walters, M. A.; Schoenen, F. J.; Lin, H. J.; Deshaies, R. J.; Arkin, M. R. Specific Inhibition of p97/VCP ATPase and Kinetic Analysis Demonstrate Interaction between D1 and D2 ATPase Domains. J Mol Biol 2014, 426, 2886-2899.

Baell, J.; Walters, M. A. Chemical con artists foil drug discovery. Nature 2014, 513, 481-483.

Yu, Y. Y.; Georg, G. I. Dehydrogenative alkenylation of uracils via palladium-catalyzed regioselective C-H activation. Chem Commun 2013, 49, 3694-3696.

Yu, Y. Y.; Bi, L.; Georg, G. I. Palladium-Catalyzed Direct C-H Arylation of Cyclic Enaminones with Aryl Iodides. J Org Chem 2013, 78, 6163-6169.

Stenland, C. J.; Lis, L. G.; Schendel, F. J.; Hahn, N. J.; Smart, M. A.; Miller, A. L.; von Keitz, M. G.; Gurvich, V. J. A Practical and Scalable Manufacturing Process for an Antifungal Agent, Nikkomycin Z. Organic Process Research & Development 2013, 17, 265-272.

Schonbrunn, E.; Betzi, S.; Alam, R.; Martin, M. P.; Becker, A.; Han, H. J.; Francis, R.; Chakrasali, R.; Jakkaraj, S.; Kazi, A.; Sebti, S. M.; Cubitt, C. L.; Gebhard, A. W.; Hazlehurst, L. A.; Tash, J. S.; Georg, G. I. Development of Highly Potent and Selective Diaminothiazole Inhibitors of Cyclin-Dependent Kinases. J Med Chem 2013, 56, 3768-3782.

Martin, M. P.; Olesen, S. H.; Georg, G. I.; Schonbrunn, E. Cyclin-Dependent Kinase Inhibitor Dinaciclib Interacts with the Acetyl-Lysine Recognition Site of Bromodomains. Acs Chem Biol 2013, 8, 2360-2365.

Kim, S. W.; Schenck, C. H.; Grant, J. E.; Yoon, G.; Dosa, P. I.; Odlaug, B. L.; Schreiber, L. R. N.; Hurwitz, T. D.; Pfausll, J. G. Neurobiology of Sexual Desire. Neuroquantology 2013, 11, 332-359.

Hutt, O. E.; Doan, T. L.; Georg, G. I. Synthesis of Skeletally Diverse and Stereochemically Complex Library Templates Derived from lsosteviol and Steviol. Org Lett 2013, 15, 1602-1605.

Gurvich, V. J.; Byrn, S. R. NIPTE: a multi-university partnership supporting academic drug development. Drug Discovery Today 2013, 18, 916-921.

Gu, X. X.; Georg, G. I. Lithium perchlorate-, acetic anhydride-, and triphenylphosphine-assisted multicomponent syntheses of 4-unsubstituted 2,5-dioxooctahydroquinoline-3-carboxylates and 3-carbonitriles. Tetrahedron 2013, 69, 9406-9416.

Georg, G. I.; Wang, S. M. Hepatitis C Virus (HCV) Therapies Special Thematic Issue: Call for Papers. J Med Chem 2013, 56, 387-387.

Dosa, P. I.; Ward, T.; Walters, M. A.; Kim, S. W. Synthesis of Novel Analogs of Cabergoline: Improving Cardiovascular Safety by Removing 5-HT2B Receptor Agonism. Acs Med Chem Lett 2013, 4, 254-258.

Dosa, P. I.; Ward, T.; Castro, R. E.; Rodrigues, C. M. P.; Steer, C. J. Synthesis and Evaluation of Water-Soluble Prodrugs of Ursodeoxycholic Acid (UDCA), an Anti-apoptotic Bile Acid. Chemmedchem 2013, 8, 1002-1011.

Dahlin, J. L.; Sinville, R.; Solberg, J.; Zhou, H.; Han, J. H.; Francis, S.; Strasser, J. M.; John, K.; Hook, D. J.; Walters, M. A.; Zhang, Z. G. A Cell-Free Fluorometric High-Throughput Screen for Inhibitors of Rtt109-Catalyzed Histone Acetylation. Plos One 2013, 8.

Chung, S. S. W.; Cuellar, R. A. D.; Wang, X. Y.; Reczek, P. R.; Georg, G. I.; Wolgemuth, D. J. Pharmacological Activity of Retinoic Acid Receptor Alpha-Selective Antagonists in Vitro and in Vivo. Acs Med Chem Lett 2013, 4, 446-450.

Bancos, I.; Bida, J. P.; Tian, D.; Bundrick, M.; John, K.; Holte, M. N.; Her, Y. F.; Evans, D.; Saenz, D. T.; Poeschla, E. M.; Hook, D.; Georg, G.; Maher, L. J., III. High-Throughput Screening for Growth Inhibitors Using a Yeast Model of Familial Paraganglioma. PLoS ONE 2013, 8, e56827.

Tash, J. S. H2-Gamendazole, a New Non-Hormonal Oral Male Contraceptive: The Road to Clinical Trials. J Androl 2012, 33, 27-27.

Sajjad, M.; Riaz, U.; Yao, R.; Bernacki, R. J.; Abouzied, M.; Erb, D. A.; Chaudhary, N. D.; Veith, J. M.; Georg, G. I.; Nabi, H. A. Investigation of 3 '-debenzoyl-3 '-(3-([I-124]-iodobenzoy))paclitaxel analog as a radio-tracer to study multidrug resistance in vivo. Appl Radiat Isotopes 2012, 70, 1624-1631.

Oglesbee, D.; Kroll, C.; Gakh, O.; Solberg, J.; Deutsch, E.; Lynch, D.; Raymond, K.; Gavrilov, D.; Tortorelli, S.; Rinaldo, P.; Matern, D.; Hook, D.; Isaya, G. A Protein-Based Assay for Population Screening and Therapeautic Drug Discovery for Friedreich Ataxia. Ann Neurol 2012, 72, S230-S230.

Niphakis, M. J.; Gay, B. C.; Hong, K. H.; Bleeker, N. P.; Georg, G. I. Synthesis and evaluation of the anti-proliferative and NF-kappa B activities of a library of simplified tylophorine analogs. Bioorgan Med Chem 2012, 20, 5893-5900.

Lis, L. G.; Smart, M. A.; Luchniak, A.; Gupta, M. L.; Gurvich, V. J. Synthesis and Biological Evaluation of a Biotinylated Paclitaxel with an Extra-Long Chain Spacer Arm. Acs Med Chem Lett 2012, 3, 745-748.

Li, M.; Shandilya, S. M. D.; Carpenter, M. A.; Rathore, A.; Brown, W. L.; Perkins, A. L.; Harki, D. A.; Solberg, J.; Hook, D. J.; Pandey, K. K.; Parniak, M. A.; Johnson, J. R.; Krogan, N. J.; Somasundaran, M.; Ali, A.; Schiffer, C. A.; Harris, R. S. First-In-Class Small Molecule Inhibitors of the Single-Strand DNA Cytosine Deaminase APOBEC3G. Acs Chem Biol 2012, 7, 506-517.

Lee, J. C.; Francis, S.; Dutta, D.; Gupta, V.; Yang, Y.; Zhu, J. Y.; Tash, J. S.; Schonbrunn, E.; Georg, G. I. Synthesis and Evaluation of Eight- and Four-Membered Iminosugar Analogues as Inhibitors of Testicular Ceramide-Specific Glucosyltransferase, Testicular beta-Glucosidase 2, and Other Glycosidases. J Org Chem 2012, 77, 3082-3098.

Kim, Y. W.; Niphakis, M. J.; Georg, G. I. Copper-Assisted Palladium(II)-Catalyzed Direct Arylation of Cyclic Enaminones with Arylboronic Acids. J Org Chem 2012, 77, 9496-9503.

Chugh, R.; Sangwan, V.; Patil, S. P.; Dudeja, V.; Dawra, R. K.; Banerjee, S.; Schumacher, R. J.; Blazar, B. R.; Georg, G. I.; Vickers, S. M.; Saluja, A. K. A Preclinical Evaluation of Minnelide as a Therapeutic Agent Against Pancreatic Cancer. Sci Transl Med 2012, 4.

Yu, Y. Y.; Niphakis, M. J.; Georg, G. I. Palladium(II)-Catalyzed Dehydrogenative Alkenylation of Cyclic Enaminones via the Fujiwara-Moritani Reaction. Org Lett 2011, 13, 5932-5935.

Selki, H.; Georg, G. I. Three-Component Synthesis of Cyclic Enaminones via Ketene Cyclization. Org Lett 2011, 13, 2147-2149.

Schneider, C. M.; Khownium, K.; Li, W.; Spletstoser, J. T.; Haack, T.; Georg, G. I. Synthesis of Oximidine II by a Copper-Mediated Reductive Ene-Yne Macrocyclization. Angew Chem Int Edit 2011, 50, 7855-7857.

Rangwala, H. S.; Giraldes, J. W.; Gurvich, V. J. Synthesis and purification of [2-C-13]-5-fluorouracil. J Labelled Compd Rad 2011, 54, 340-343.

Pepe, A.; Pamment, M.; Georg, G. I.; Malhotra, S. V. Synthesis of Fused Bicyclic Systems with Nitrogen Atom at the Bridgehead, Including Indolizidines and Quinolizidines. J Org Chem 2011, 76, 3527-3530.

Niphakis, M. J.; Georg, G. I. Synthesis of Tylocrebrine and Related Phenanthroindolizidines by VOF3-Mediated Oxidative Aryl-Alkene Coupling. Org Lett 2011, 13, 196-199.

Leighty, M. W.; Spletstoser, J. T.; Georg, G. I.; Umihara, H.; Fukuyama, T. Mild conversion of tertiary amides to aldehydes using Cp2Zr(H)Cl (Schwartz's reagent). Organic Syntheses 2011, 88, 427-437.

Leighty, M. W.; Georg, G. I. Total Syntheses and Cytotoxicity of (R)- and (S)-Boehmeriasin A. Acs Med Chem Lett 2011, 2, 313-315.

Gupta, V. G.; Zelinski, M.; Steinmetz, K.; Miklos, A.; Broward, M.; Jakkaraj, S.; Chakrasali, R.; Georg, G. I.; Tash, J. S. Anti-Spermatogenic Efficacy of Nonhormonal Male Contraceptive Agent, H2-Gamendazole, in Mice, Rats, Rabbits, and Nonhuman Primates (Rhesus), and a Multiple Low Dose Oral Regimen That Gives 100% Infertility with Complete Reversibility. Biol Reprod 2011, 85.

Doan, T. L.; Pollastri, M.; Walters, M. A.; Georg, G. I. The Future of Drug Repositioning: Old Drugs, New Opportunities. Annu Rep Med Chem 2011, 46, 385-401.

Bi, L.; Georg, G. I. Direct Hiyama Cross-Coupling of Enaminones With Triethoxy(aryl)silanes and Dimethylphenylsilanol. Org Lett 2011, 13, 5413-5415.

Betzi, S.; Alam, R.; Martin, M.; Lubbers, D. J.; Han, H. J.; Jakkaraj, S. R.; Georg, G. I.; Schonbrunn, E. Discovery of a Potential Allosteric Ligand Binding Site in CDK2. Acs Chem Biol 2011, 6, 492-501.

Benyumov, A.; Gurvich, V. J.; Lis, L. G.; Williams, B. W.; Kirstein, M. N. Combinatorial Pharmacologic Effects of Gemcitabine and its Metabolite dFdU. Chemmedchem 2011, 6, 457-464.

Seki, H.; Georg, G. I. Synthesis of Amino Acid Derived Enaminones via Wolff Rearrangement Using Vinylogous Amides as Carbon Nucleophiles. J Am Chem Soc 2010, 132, 15512-15513.

Reiff, E. A.; Nair, S. K.; Henri, J. T.; Greiner, J. F.; Reddy, B. S.; Chakrasali, R.; David, S. A.; Chiu, T. L.; Amin, E. A.; Himes, R. H.; Vander Velde, D. G.; Georg, G. I. Total Synthesis and Evaluation of C26-Hydroxyepothilone D Derivatives for Photoaffinity Labeling of beta-Tubulin. J Org Chem 2010, 75, 86-94.

Podolyan, Y.; Walters, M. A.; Karypis, G. Assessing Synthetic Accessibility of Chemical Compounds Using Machine Learning Methods. J Chem Inf Model 2010, 50, 979-991.

Niphakis, M. J.; Turunen, B. I.; Georg, G. I. Synthesis of 6-and 7-Membered Cyclic Enaminones: Scope and Mechanism. J Org Chem 2010, 75, 6793-6805.

Niphakis, M. J.; Georg, G. I. Total Syntheses of Arylindolizidine Alkaloids (+)-Ipalbidine and (+)-Antofine. J Org Chem 2010, 75, 6019-6022.

Hutt, O. E.; Inagaki, J.; Reddy, B. S.; Nair, S. K.; Reiff, E. A.; Henri, J. T.; Greiner, J. F.; VanderVelde, D. G.; Chiu, T. L.; Amin, E. A.; Himes, R. H.; Georg, G. I. Total synthesis and evaluation of 22-(3-azidobenzoyloxy)methyl epothilone C for photoaffinity labeling of beta-tubulin. Bioorg Med Chem Lett 2009, 19, 3293-3296.

Holets, L.; Jakkaraj, S.; Chakrasali, R.; Georg, G. I.; Tash, J. S. Effect of Gamendazole on Expression of Heat Shock Proteins HSP70 and HSP90 in Rat Testis and Primary Sertoli Cells. Biol Reprod 2009, 76-76.

Desino, K. E.; Ansar, S.; Georg, G. I.; Himes, R. H.; Michaelis, M. L.; Powell, D. R.; Reiff, E. A.; Telikepalli, H.; Audus, K. L. (3R,5S,7as)-(3,5-Bis(4-fluorophenyl)tetrahydro-1H-oxazolo[3,4-c]oxazol-7a-yl)methanol, a Novel Neuroprotective Agent. J Med Chem 2009, 52, 7537-7543.

Chugh, R.; Patil, S.; Dudeja, V.; Borja-Cacho, D.; Dawra, R.; Yokoyama, Y.; Mujumdar, N.; Antonoff, M.; Clawson, K.; Vickers, S.; Georg, G.; Saluja, A. Minnelide: A Novel Therapeutic Strategy Against Pancreatic Cancer. Pancreas 2009, 38, 989-989.

Chiu, T. L.; Solberg, J.; Patil, S.; Geders, T. W.; Zhang, X.; Rangarajan, S.; Francis, R.; Finzel, B. C.; Walters, M. A.; Hook, D. J.; Amin, E. A. Identification of Novel Non-Hydroxamate Anthrax Toxin Lethal Factor Inhibitors by Topomeric Searching, Docking and Scoring, and in Vitro Screening. J Chem Inf Model 2009, 49, 2726-2734.

Tash, J. S.; Chakrasali, R.; Jakkaraj, S. R.; Hughes, J.; Smith, S. K.; Hornbaker, K.; Heckert, L. L.; Ozturk, S. B.; Hadden, M. K.; Kinzy, T. G.; Blagg, B. S. J.; Georg, G. I. Gamendazole, an orally active indazole carboxylic acid male contraceptive agent, targets HSP90AB1 (HSP90BETA) and EEF1A1 (eEF1A), and stimulates Il1a transcription in rat sertoli cells. Biol Reprod 2008, 78, 1139-1152.

Tash, J. S.; Attardi, B.; Hild, S. A.; Chakrasali, R.; Jakkaraj, S. R.; Georg, G. I. A novel potent indazole carboxylic acid derivative blocks spermatogenesis and is contraceptive in rats after a single oral dose. Biol Reprod 2008, 78, 1127-1138.

Tash, J. Gamendazole: A potent antispermatogenic contraceptive agent with novel targets Hsp90 beta and eEF1A. Biol Reprod 2008, 91-91.

Ge, H. B.; Niphakis, M. J.; Georg, G. I. Palladium(II)-catalyzed direct arylation of enaminones using organotrifluoroborates. J Am Chem Soc 2008, 130, 3708-+.

Cotitta, J.; Ozturk, S.; Kinzy, T.; Jakkaraj, S.; Chakrasali, R.; Gross, S.; Georg, G.; Tash, J. The candidate male contraceptive agent, gamendazole, affects actin organization and vinculin based focal contact distribution in sertoli cells in vitro. Biol Reprod 2008, 206-207.